3 documents found, page 1 of 1
Semi-synthesis of small molecules of aminocarbazoles: Tumor growth inhibition a...
Long, S; Loureiro, JB; Carvalho, C; Gales, L; Saraiva, L; Pinto, MMM; Puthongking, P; Sousa, EThe tumor suppressor p53 is inactivated by mutation in approximately 50% of human cancers. Small molecules that bind and stabilize those mutants may represent effective anticancer drugs. Herein, we report the tumor cell growth inhibitory activity of carbazole alkaloids and amino derivatives, as well as their potential activation of p53. Twelve aminocarbazole alkaloids were semi-synthesized from heptaphylline (1...
Targeting p53 for melanoma treatment: Counteracting tumour proliferation, disse...
Loureiro, JB; Raimundo, L; Calheiros, J; Carvalho, C; Barcherini, V; Lima, NR; Gomes, C; Almeida, MI; Alves, MG; Costa, JL; Santos, MMM; Saraiva, LMelanoma is the deadliest form of skin cancer, primarily due to its high metastatic propensity and therapeutic resistance in advanced stages. The frequent inactivation of the p53 tumour suppressor protein in melanomagenesis may predict promising outcomes for p53 activators in melanoma therapy. Herein, we aimed to investigate the antitumor potential of the p53-activating agent SLMP53-2 against melanoma. Two-and ...
SLMP53-2 restores wild-type-like function to mutant p53 through hsp70: Promisin...
Gomes, S; Bosco, B; Loureiro, JB; Ramos, H; Raimundo, L; Soares, J; Nazareth, N; Barcherini, V; Domingues, L; Oliveira, C; Bisio, A; Piazza, SHalf of human cancers harbor TP53 mutations that render p53 inactive as a tumor suppressor. In these cancers, reactivation of mutant p53 (mutp53) through restoration of wild-type-like function constitutes a valuable anticancer therapeutic strategy. In order to search for mutp53 reactivators, a small library of tryptophanol-derived oxazoloisoindolinones was synthesized and the potential of these compounds as mut...